PH12015502246A1 - Benzimidazolone derivatives as bromodomain inhibitors - Google Patents

Benzimidazolone derivatives as bromodomain inhibitors

Info

Publication number
PH12015502246A1
PH12015502246A1 PH12015502246A PH12015502246A PH12015502246A1 PH 12015502246 A1 PH12015502246 A1 PH 12015502246A1 PH 12015502246 A PH12015502246 A PH 12015502246A PH 12015502246 A PH12015502246 A PH 12015502246A PH 12015502246 A1 PH12015502246 A1 PH 12015502246A1
Authority
PH
Philippines
Prior art keywords
compounds
bromodomain inhibitors
benzimidazolone derivatives
bromodomain
inhibitors
Prior art date
Application number
PH12015502246A
Inventor
Aktoudianakis Evangelos
Chin Gregory
Corkey Britton Kenneth
Du Jinfa
Elbel Kristyna
Robert H Jiang
Kobayashi Tetsuya
Martinez Ruben
Samuel E Metobo
Mish Michael
Shevick Sophie
Sperandio David
Yang Hai
Zablocki Jeff
Original Assignee
Gilead Sciences Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Gilead Sciences Inc filed Critical Gilead Sciences Inc
Publication of PH12015502246A1 publication Critical patent/PH12015502246A1/en

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Epidemiology (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula (I) wherein R1a, R1b, R2a, R2b, R3, and X are described herein.
PH12015502246A 2013-03-28 2015-09-24 Benzimidazolone derivatives as bromodomain inhibitors PH12015502246A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361805995P 2013-03-28 2013-03-28
US201361860230P 2013-07-30 2013-07-30
PCT/US2014/032031 WO2014160873A1 (en) 2013-03-28 2014-03-27 Benzimidazolone derivatives as bromodomain inhibitors

Publications (1)

Publication Number Publication Date
PH12015502246A1 true PH12015502246A1 (en) 2016-02-01

Family

ID=50897885

Family Applications (1)

Application Number Title Priority Date Filing Date
PH12015502246A PH12015502246A1 (en) 2013-03-28 2015-09-24 Benzimidazolone derivatives as bromodomain inhibitors

Country Status (35)

Country Link
US (2) US9255089B2 (en)
EP (1) EP2978759B1 (en)
JP (1) JP6339175B2 (en)
KR (1) KR101847698B1 (en)
CN (1) CN105102453B (en)
AP (1) AP2015008741A0 (en)
AU (1) AU2014241152B2 (en)
BR (1) BR112015024078A2 (en)
CA (1) CA2907502C (en)
CL (1) CL2015002871A1 (en)
CR (1) CR20150515A (en)
CY (1) CY1119165T1 (en)
DK (1) DK2978759T3 (en)
EA (1) EA029497B1 (en)
ES (1) ES2626397T3 (en)
HK (1) HK1220692A1 (en)
HR (1) HRP20170750T1 (en)
HU (1) HUE034772T2 (en)
IL (1) IL241186A0 (en)
LT (1) LT2978759T (en)
MD (1) MD4531C1 (en)
MX (1) MX2015013798A (en)
MY (1) MY176634A (en)
NZ (1) NZ711586A (en)
PE (1) PE20151982A1 (en)
PH (1) PH12015502246A1 (en)
PL (1) PL2978759T3 (en)
PT (1) PT2978759T (en)
RS (1) RS56050B1 (en)
SG (1) SG11201507926RA (en)
SI (1) SI2978759T1 (en)
TW (1) TWI530499B (en)
UY (1) UY35516A (en)
WO (1) WO2014160873A1 (en)
ZA (1) ZA201506356B (en)

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NZ714669A (en) 2013-06-21 2021-07-30 Zenith Epigenetics Ltd Novel bicyclic bromodomain inhibitors
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EA201690087A1 (en) 2013-07-31 2016-08-31 Зенит Эпидженетикс Корп. NEW QUINAZOLINONS AS BROMOMODENIAL INHIBITORS
US9315501B2 (en) 2013-11-26 2016-04-19 Incyte Corporation Bicyclic heterocycles as BET protein inhibitors
WO2015081203A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
WO2015095492A1 (en) 2013-12-19 2015-06-25 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
SG11201608843TA (en) 2014-04-23 2016-11-29 Incyte Corp 1H-PYRROLO[2,3-c]PYRIDIN-7(6H)-ONES AND PYRAZOLO[3,4-c]PYRIDIN-7(6H)-ONES AS INHIBITORS OF BET PROTEINS
WO2016044130A1 (en) 2014-09-15 2016-03-24 Incyte Corporation Tricyclic heterocycles for use as bet protein inhibitors
JP6930913B2 (en) 2014-10-14 2021-09-01 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニアThe Regents Of The University Of California Usage of CDK9 and BRD4 inhibitors to inhibit inflammation
CA2966303A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Ltd. Substituted pyridines as bromodomain inhibitors
WO2016087936A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Corp. Substituted pyridinones as bromodomain inhibitors
CA2966449A1 (en) 2014-12-11 2016-06-16 Zenith Epigenetics Ltd. Substituted heterocycles as bromodomain inhibitors
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KR102662814B1 (en) 2015-03-13 2024-05-03 리스버로직스 코퍼레이션 Compositions and treatment methods for treating complement-related diseases
GB201504689D0 (en) 2015-03-19 2015-05-06 Glaxosmithkline Ip Dev Ltd Chemical compounds
GB201504694D0 (en) 2015-03-19 2015-05-06 Glaxosmithkline Ip Dev Ltd Covalent conjugates
WO2016203335A1 (en) 2015-06-18 2016-12-22 Pfizer Inc. Novel pyrido[2,3-b]pyrazinones as bet-family bromodomain inhibitors
US20170121347A1 (en) 2015-10-29 2017-05-04 Incyte Corporation Amorphous solid form of a bet protein inhibitor
WO2017114843A1 (en) 2015-12-29 2017-07-06 INSERM (Institut National de la Santé et de la Recherche Médicale) Xanthine derivative inhibitors of bet proteins
IL263824B2 (en) 2016-06-20 2023-10-01 Incyte Corp Crystalline solid forms of a bet inhibitor
WO2018097976A1 (en) * 2016-11-22 2018-05-31 Gilead Sciences, Inc. Synthesis of a compound that modulates the activity of bromodomain-containing proteins
CA3081753A1 (en) 2017-11-06 2019-05-09 Centre National De La Recherche Scientifique Xanthine derivatives and uses thereof as inhibitors of bromodomains of bet proteins
SG11202005793SA (en) * 2017-12-20 2020-07-29 Betta Pharmaceuticals Co Ltd Compound functioning as bromodomain protein inhibitor, and composition
EP3919127A4 (en) * 2019-02-02 2022-12-07 CSPC Zhongqi Pharmaceutical Technology (Shijiazhuang) Co., Ltd. Targeted ubiquitination degradation brd4 protein compound, preparation method therefor and application thereof
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Also Published As

Publication number Publication date
HK1220692A1 (en) 2017-05-12
ES2626397T3 (en) 2017-07-24
HUE034772T2 (en) 2018-02-28
KR20150135476A (en) 2015-12-02
EP2978759B1 (en) 2017-03-15
MX2015013798A (en) 2016-02-16
NZ711586A (en) 2016-09-30
MD4531B1 (en) 2017-11-30
EP2978759A1 (en) 2016-02-03
AU2014241152A1 (en) 2015-09-17
PL2978759T3 (en) 2017-08-31
CL2015002871A1 (en) 2016-05-13
US20160031868A1 (en) 2016-02-04
IL241186A0 (en) 2015-11-30
SI2978759T1 (en) 2017-05-31
BR112015024078A2 (en) 2017-07-18
JP2016515584A (en) 2016-05-30
TW201504233A (en) 2015-02-01
CY1119165T1 (en) 2018-02-14
ZA201506356B (en) 2017-08-30
UY35516A (en) 2014-09-30
RS56050B1 (en) 2017-09-29
AU2014241152B2 (en) 2016-11-03
TWI530499B (en) 2016-04-21
US9255089B2 (en) 2016-02-09
EA029497B1 (en) 2018-04-30
WO2014160873A1 (en) 2014-10-02
MD20150104A2 (en) 2016-02-29
MD4531C1 (en) 2018-06-30
CA2907502C (en) 2018-02-27
CN105102453B (en) 2018-04-06
KR101847698B1 (en) 2018-04-10
HRP20170750T1 (en) 2017-07-28
CN105102453A (en) 2015-11-25
DK2978759T3 (en) 2017-06-19
MY176634A (en) 2020-08-19
PE20151982A1 (en) 2016-01-28
PT2978759T (en) 2017-05-31
EA201591455A1 (en) 2016-01-29
JP6339175B2 (en) 2018-06-06
AP2015008741A0 (en) 2015-09-30
CA2907502A1 (en) 2014-10-02
US20140296246A1 (en) 2014-10-02
SG11201507926RA (en) 2015-10-29
CR20150515A (en) 2015-12-01
LT2978759T (en) 2017-05-25

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